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Salirasib

CAS No. : 162520-00-5

MCE 国际站：Salirasib

产品活性：Salirasib是一种 Ras 抑制剂，可特异性抑制致癌激活的Ras和生长因子受体介导的Ras激活，从而抑制Ras依赖性肿瘤生长。

研究领域：GPCR/G Protein  |  Autophagy

作用靶点：Ras  |  Autophagy

In Vitro: Salirasib (12.5-100 μM) inhibits the proliferation of ELT3 cells in a dose-dependent manner with an average IC₅₀ of 58.57±4.59 μM. The effects of Salirasib on the TSC2-null cells are evidently mimicked by DN-Rheb but not by DN-Ras. Salirasib reduces Rheb in TSC2-null cells and TSC2 expression rescues the cells from the inhibitory effect of Salirasib. Salirasib reduces phosphorylation of S6K but not of ERK in the TSC2-null ELT3 cells. Salirasib (50, 100, 150 μM) induces a dose- and time-dependent decrease of cell growth in HCC cells. Salirasib reduces cell proliferation through modulation of cell cycle effectors and inhibitors. Salirasib induces apoptosis in HepG2 and Hep3B cells. The growth inhibitory effect of salirasib in HCC cell lines is associated with mTOR inhibition independent of ERK or Akt activation.

In Vivo: Salirasib (40, 60 or 80 mg/kg, p.o.) significantly inhibits the tumor growth in a dose dependent manner in vivo. Salirasib (5 mg/kg, i.p.) significantly decreases Ras expression in the dy^2J/dy^2Jmice, and causes an increase in Ras expression which is by far much lower than the increase observed in the dy^2J/dy^2J mice. Salirasib treatment is associated with significantly inhibition of both MMP-2 and MMP-9 activities in the dy^2J/dy^2J mice. Salirasib (10 mg/kg, i.p.) inhibits tumour growth in a subcutaneous xenograft mice model without weight loss.

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